Assay Detail
Functional
CHEMBL5364540
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Bronchoconstriction activity in Sprague-Dawley rat trachea assessed as inhibition of carbachol-induced tracheal contraction
10
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Trachea |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Optimization of M<sub>3</sub> Antagonist-PDE4 Inhibitor (MAPI) Dual Pharmacology Molecules for the Treatment of COPD.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.06 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5426968 | — | — | 1 | 9.00 |
| CHEMBL5395712 | — | — | 2 | 8.60 |
| CHEMBL5408238 | — | — | 2 | 8.40 |
| CHEMBL5409010 | — | — | 1 | 8.40 |
| CHEMBL5417689 | — | — | 1 | 7.90 |
| CHEMBL5399363 | — | — | 2 | 7.80 |
| CHEMBL5410533 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5426968 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5395712 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL5395712 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL5408238 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5409010 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5417689 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL5399363 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5410533 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL5408238 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5399363 | — | IC50 | = | 100.0 | nM | 7.00 |